反应详情

To a solution of piperonylic acid (0.500 g, 3.01 mmol), EDC (0.867 g, 4.52 mmol), HOBT (0.611 g, 4.52 mmol) in anhydrous DMF (10 mL) was added a solution of TEA (1.67 mL, 12.04 mmol), 3-Amino-4-(3,5-difluoro-phenyl)-1-(3-ethyl-benzylamino)-butan-2-ol (1.693 g, 3.01 mmol), and anhydrous DMF (5 mL). Reaction mixture was stirred under nitrogen overnight. Quenched reaction mixture with 10% sodium bicarbonate (aq.) then extracted with ethyl acetate. Washed organic layer with 1N HCl, followed by a wash with 10% sodium bicarbonate (aq.). Dried organic layer over magnesium sulfate, filtered, then concentrated in vacuo, yielding the product. (ES+: 483.2)

1. customReaction mixture
2. customQuenched
3. customreaction mixture with 10% sodium bicarbonate (aq.)
4. extractionthen extracted with ethyl acetate
5. washa wash with 10% sodium bicarbonate (aq.)
6. filtrationDried organic layer over magnesium sulfate, filtered
7. concentrationconcentrated in vacuo
8. customyielding the product